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Titolo:
INTERACTION OF 5 HT1B D LIGANDS WITH RECOMBINANT-H 5-HT1A RECEPTORS -INTRINSIC ACTIVITY AND MODULATION BY G-PROTEIN ACTIVATION STATE/
Autore:
PAUWELS PJ; PALMIER C; DUPUIS DS; COLPAERT FC;
Indirizzi:
CTR RECH PIERRE FABRE,DEPT MOL & CELLULAR BIOL,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 5, volume: 357, anno: 1998,
pagine: 490 - 499
SICI:
0028-1298(1998)357:5<490:IO5HDL>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADENYLATE-CYCLASE; ALPHA-SUBUNITS; PARTIAL AGONISTS; SEROTONIN; BINDING; IDENTIFICATION; PHARMACOLOGY; HIPPOCAMPUS; EXPRESSION; POTENT;
Keywords:
RECOMBINANT H 5-HT1A RECEPTOR; [S-35] GTP-GAMMA-S BINDING RESPONSE; 5-HT1B/D AGONISTS; LIGAND EFFICACY; C6-GLIAL AND HELA CELL LINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Pauwels et al., "INTERACTION OF 5 HT1B D LIGANDS WITH RECOMBINANT-H 5-HT1A RECEPTORS -INTRINSIC ACTIVITY AND MODULATION BY G-PROTEIN ACTIVATION STATE/", Naunyn-Schmiedeberg's archives of pharmacology, 357(5), 1998, pp. 490-499

Abstract

Many 5-HT1B/D receptor ligands have affinity for 5-HT1A receptors. Inthe present study, the intrinsic activity of a series of 5-HT1B/D ligands was investigated at human 5-HT1A (h 5-HT1A) receptors by measuring G-protein activation in recombinant C6-glial and HeLa membranes, using agonist-stimulated [S-35]GTP gamma S binding. In these two mem brane preparations, the density of h 5-HT1A receptors (i.e., 246 to 320 fmol mg(-1) protein) and of their G-proteins, and the receptor: G-protein density ratio (0.08 to 0.18) appeared to be similar. It was found that: (i) the maximal [S-35]GTP gamma S binding responses induced by the5-HT1B/D receptor ligands in the HeLa preparation at 30 mu M GDP werecomparable to that of the native agonist 5-HT; (ii) as compared to 5-HT (1.00), similar potencies but lower maximal responses were observedin the C6-glial preparation at 0.3 mu M GDP for zolmitriptan (0.89), dihydroergotamine (0.81), rizatriptan (0.71), CP122638 (0.69), naratriptan (0.60) and sumatriptan (0.53); and that (iii) maximal [S-35]GTP gamma S binding responses induced by 5-HT1B/D ligands in the C6-glial preparation were either unaffected or significantly enhanced by increasing the GDP concentration from 0.3 to 30 mu M and higher concentrations. These features differ from those observed with 5-HT1A receptor agonists; the latter display the same rank order of potency and efficacy in both membrane preparations, and increasing the amount of GDP with CG-glial membranes results in an attenuation of both the agonist's maximal effect and the apparent potency of partial agonists. The differential regulation of 5-HT1A and 5-HT1B/D agonist responses by GDP suggeststhat different G-protein subtypes are involved upon 5-HT1A receptor activation by 5-HT1A and 5-HT1B/D agonists.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 19:52:47